Neratinib

Synonym
Product Category
Product Code
CAS Number
MDL Number
Pubchem CID
Reaxys RN
HKI-272, PB-272
API & Intermediates
KAPI0F20
698387-09-6
MFCD09752958
9915743
9971763
image-155171-Trimethyl(trifluoromethyl)silane_reagent.png
Chemical Name
Molecular Formula
Molecular Weight
Assay
Appearance
Melting Point
Packaging
Storage
Neratinib
C30H29ClN6O3
557.04
≥99%(HPLC)
Light Yellow to Yellow Solid
178-183°C
500mg,1g,10g,25g,50g,100g and 500g
-20°C Freezer
Neratinib (also known as HKI-272, PB-272) is an orally irreversible tyrosine kinase inhibitor with activity against HER2 and EGFR kinases for the treatment of breast and non-small cell lung cancer.
Efficacy and safety of trastuzumab as a single agent in first-line treatment of HER2-overexpressing metastatic breast cancer. [1]
Antitumor activity of HKI-272, an orally active, irreversible inhibitor of the HER-2 tyrosine kinase. [2]
Molecular mechanisms of epidermal growth factor receptor (EGFR) activation and response to gefitinib and other EGFR-targeting drugs. [3]
Second-Generation Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors in Non-Small Cell Lung Cancer. [4]
HER2 directed small molecule antagonists. [5]
Comprehensive analysis of kinase inhibitor selectivity. [6]
HER2 activating mutations are targets for colorectal cancer treatment. [7]
Efficacy and mechanism of action of the tyrosine kinase inhibitors gefitinib, lapatinib and neratinib in the treatment of HER2-positive breast cancer: preclinical and clinical evidence. [8]
References:
[1] C.L.Vogel, et al, J. Clin. Oncol., 2002, 20(3), pp 719-726.
[2] S.K.Rabindran, et al, Cancer Res., 2004, 64(11), pp 3958-3965.
[3] M.Ono, et al, Clin. Cancer Res., 2006, 12(24), pp 7242-7251.
[4] L.V.Sequist, Oncologist, 2007, 12(3), pp 325-330.
[5] M.Arkin, et al, Curr. Opin. Investig. Drugs, 2008, 9(12), pp 1264-1276.
[6] M.Z.Davis, et al, Nat. Biotechmol., 2011, 29(11), pp 1046-1051.
[7] S.M.Kavuri, et al, Cancer Discov., 2015, 5(8), pp 832-841.
[8] M.Segovia-Mendoza, et al, Am. J. Cancer Res., 2015, 5(9), pp 2531-2561.
Signal Word
Hazard Statements
Precautionary Statements
HS Code
RIDADR
Legal Information
Warning
P361
P201,P202,P281,P308+P313

NONH for all modes of transport
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